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Bioorg Med Chem Lett ; 26(10): 2455-2458, 2016 05 15.
Article in English | MEDLINE | ID: mdl-27072906

ABSTRACT

We have developed the practical method for polyfluorosalicylic acids synthesis via nucleophilic ortho-mono-substitution of fluorine atom with magnesium methoxide. We have managed to increase the yield of targeted polyfluorosalicylic acids from good to quantitative. We have studied the tuberculostatic activity of polyfluorosalicylic acids. It has been found that minimum inhibitory concentration (MIC) of compounds is from 0.7 to 6.5µg/mL depending on the structure.


Subject(s)
Antitubercular Agents/chemistry , Antitubercular Agents/pharmacology , Antitubercular Agents/chemical synthesis , Chemistry Techniques, Synthetic , Drug Evaluation, Preclinical/methods , Fluorine/chemistry , Magnesium Compounds/chemistry , Microbial Sensitivity Tests , Molecular Structure , Mycobacterium tuberculosis/drug effects , Salicylic Acid/chemistry
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